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Methodology for Identification of Cysteine-Reactive Covalent Inhibitors

  • Stefan G. Kathman
  • Alexander V. Statsyuk
Protocol
Part of the Methods in Molecular Biology book series (MIMB, volume 1967)

Abstract

Covalent fragments are an emerging technology to discover covalent ligands in target-based or phenotypic screens. Here we describe screening of cysteine-reactive covalent fragments against a protein of interest using mass spectrometry or enzymatic methods.

Key words

Covalent fragments Cysteine 

Notes

Acknowledgments

Funding was provided from Northwestern University (A.V.S.), Pew Charitable Trusts (A.V.S.), National Institutes of Health Grants R01GM115632 (A.V.S.), T32GM105538 (S.G.K.), and the ACS Medicinal Chemistry Predoctoral Fellowship (S.G.K.). We thank Rama Mishra and the Center for Molecular Innovation and Drug Discovery for assisting with the initial design of the library of electrophilic fragments.

References

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2019

Authors and Affiliations

  • Stefan G. Kathman
    • 1
  • Alexander V. Statsyuk
    • 2
  1. 1.Northwestern University, Department of Chemistry, Silverman HallEvanstonUSA
  2. 2.University of Houston, College of PharmacyHoustonUSA

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